Cocaine is a drug with a powerful stimulating effect that increases alertness (reduces fatigue), increases concentration, reduces appetite, increases physical resistance, and may induce a state of well being or euphoria.
Cocaine may be taken orally, inhaled nasally in powdered form, or injected, usually, directly in a vein. When heated with sodium bicarbonate, it is converted into a base called crack, which may be smoked.
Cocaine increases the blood pressure and the heart rate and may cause a fatal heart attack Other effects include gastrointestinal disorders, intestinal damage, intense nervousness, a sensation that something is moving under the skin, epileptic attacks, hallucinations, sleep disorders, paranoid delirium, and violent behavior.
Due to the fact that the effects of cocaine are of short duration, ca. 30 minutes, cocaine users usually take repeated doses of the drug. To reduce some of the extreme nervousness caused by cocaine, many addicts use heroin or nervous system depressants, for example, alcohol.
Cocaine withdrawal syndrome is a syndrome which develops in cocaine addicts who stop using cocaine. The reactions typical of this syndrome include extreme fatigue and depression, i.e., reactions opposite the effects of the drug, and, frequently, suicidal tendencies appear upon discontinuation of use of the drug.
Cocaine dependency is usually treated, initially, by a psychosocial treatment. However, patients or individuals with severe forms of cocaine dependency that do not respond to said psychosocial treatment may be subjected to a pharmacological treatment. Currently, no truly effective treatment is available for cocaine withdrawal syndrome.
A review of the various pharmacological treatments to reduce the symptoms of cocaine dependency and to combat cocaine withdrawal syndrome can be found in “Practice Guideline for the Treatment of Patients With Substance Use Disorders: Alcohol, Cocaine and Opioids”, produced by the Work Group On Substance Use Disorders of the American Psychiatric Association and published in Am. J. Psychiatry 152:11, Nov. 1995 Supplement, pp. 36–39.
This publication states that approximately 20 different pharmaceutical products have been studied for the purpose of finding an effective pharmacological treatment for cocaine dependency, although there is still no truly effective treatment available. The most promising results seem to have been obtained with desipramine and amantadine although there are studies that could not confirm the positive expectations created, possibly due to differences in the cocaine addict population and the route of administration of the drug. Other pharmaceuticals tested have been carbamazepine, pergolide, carbidopalL-dopa, fluoxetine, flupenthixol, bupropion, maprolitine, phenelzine, buprenorphine, and methadone.
Likewise, the above referenced publication states that treatment with dopamine agonists, for example, amantadine, reduces the symptoms of cocaine withdrawal syndrome, although two later studies could not confirm these results. Initial studies with bromocriptine yielded some results in the treatment of cocaine withdrawal syndrome that were also not subsequently confirmed. In fact, Moscoviz et al., J. Gen. Intern. Med. 1993, 8:1–4, did not find a significant reduction between bromocriptine and placebo in outpatients.
In none of the reviews mentioned is the use of flumazenil considered in the treatment of cocaine dependency.
Flumazenil[ethyl8-fluoro-5,6-dihydro-5-methyl-6-oxo-4H-imidazol[1,5-a][1,4]benzodiazepine-3-carboxylate] is a benzodiazepine antagonist which selectively blocks the effects exerted on the central nervous system via the benzodiazepine receptors. This active principle is indicated to neutralize the central sedative effect of the benzodiazepines; consequently, it is regularly used in anesthesia to end the general anesthesia induced and maintained with benzodiazepines in hospitalized patients, or to stop the sedation produced with benzodiazepines in patients undergoing brief diagnostic or therapeutic procedures on an inpatient or outpatient basis.